Labeling with 131I of chloroquine-analogues for the detection of ocular melanoma

Bakker, C. N. M.; Kaspersen, Frans M.

doi:10.1002/jlcr.2580150181

Cited by 10 publications

(4 citation statements)

References 17 publications

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“…Triiodothyronine [239], p-iodophenyltrimethylammonium salts [240], 2-iodomorphine [241], and thiouracil derivatives [242] were prepared with specific activities of 25 to 1700 Ci/mmole. High yields were also found in the radioiodination of chloroquinoline analogs, but a high amount of chlorinated side products were also observed [243,244], This chlorination side reaction was also pointed out in another study [245]. It is interesting to note that the n.c.a.…”

Section: Direct Electrophilic Halogenationmentioning

confidence: 75%

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No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

1983

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Radiolabeling methods with the heavy halogens bromine, iodine and astatine are reviewed. The methods are evaluated on the basis of their underlying chemical principles and their usefulness for the no-carrier-added labeling of biologically-useful compounds. Special emphasis is placed on the stability, specific activity, and quality control of radiohalogenation products using the shortlived, neutron-deficient nuclides 7s ' 7 'Br, '"I, and 2 "At in view of their importance as radiopharmaceuticals.

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Section: Direct Electrophilic Halogenationmentioning

confidence: 75%

“…With respect to the side reactions of the N-chloro compounds, chlorination of the substrate is the most prédomi-nent [173,215,222,[243][244][245]248], although it is generally slower than bromination and iodination. Oxidative destruction of the target molecule is also possible, although relatively slow [248,249].…”

Section: Direct Electrophilic Halogenationmentioning

confidence: 99%

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

1983

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“…While some of the compounds have been reported in the literature, i.e. (1), 23 (2), 24 (3), 25 and (6), 23 no crystal structures have been reported for these derivatives; comprehensive spectroscopic data are collected in the ESI. † The influence of the nature of the R group upon supramolecular aggregation in these structures along with those available in the literature is investigated.…”

Section: Resultsmentioning

confidence: 99%

Assessing the persistence of the N–H⋯N hydrogen bonding leading to supramolecular chains in molecules related to the anti-malarial drug, chloroquine

et al. 2009

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Crystal packing patterns for a range of chloroquine derivatives have been investigated. For species where the amine-bound R substituent carries atoms not capable of forming significant hydrogen bonding interactions, i.e. R ¼ methyl (1), n-propyl (2), n-butyl (3), 2-chloroethyl (4), 2-azidoethyl (5), N-H/N hydrogen bonding between the amine and pyridine groups predominate leading to supramolecular chains. In species carrying hydroxyl groups, i.e. R ¼ 2-hydroxylethyl ( 6), 1-butanol (7), and (S)-1-butanol ( 8), the N-H/N interactions are subverted by O-H/N and N-H/O hydrogen bonding that results in the formation of 2-D arrays, establishing an hierarchy of hydrogen bonding interactions in these systems. Despite the differences in hydrogen bonding, globally, the crystal packing in all structures is similar in that the N-H/N mediated supramolecular chains of (1-5) aggregate into layers usually via C-H/p, C-Cl/p and p/p interactions. These layers, as with those formed in (6-8), stack into a 3-D arrangement being consolidated via C-H/Cl and p/p or C-Cl/p interactions.

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“…As mentioned, 150 µg of oxidizing agent no significant increase in the radiochemical yield of 125 ITB was obtained. Excess of oxidizing agent is not recommended in this labeling reaction to avoid a number of undesirable side reactions including chlorination …”

Section: Resultsmentioning

confidence: 99%

Iodine‐125‐terbutaline (¹²⁵ITB): a new β₂‐adrenoceptor probe for lung imaging

Amin¹

2012

Labelled Comp Radiopharmac

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Development of a selective b 2 -adrenoceptor tracer for single photon emission tomography is important for imaging of the lungs. Iodine-125-terbutaline ( 125 ITB) was prepared by the reaction of terbutaline with iodine-125 in the presence of chloramine-T as the oxidizing agent. The reaction was completed by incubation of the reaction mixture at 70 C for 15 minutes at pH 7. The biodistribution study in mice indicated the ability of the tracer to bind b-adrenoceptors in lungs, liver, heart, and spleen. The localization of the tracer in the lungs was high (85%/g at 60 minutes post-injection) and the highest lung/blood/g ratio was 19.8% at 60 minutes post-injection. The selectivity of the tracer for the b 2 -adrenoceptor was examined by blocking with both b 1 and b 2 -adrenoceptor selective antagonists. The results showed reduction of both heart and lung uptake of the 125 ITB tracer, indicating a moderate (not absolute) selectivity for the b 2 -adrenoceptor.

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Labeling with 131I of chloroquine-analogues for the detection of ocular melanoma

Cited by 10 publications

References 17 publications

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

Assessing the persistence of the N–H⋯N hydrogen bonding leading to supramolecular chains in molecules related to the anti-malarial drug, chloroquine

Iodine‐125‐terbutaline (¹²⁵ITB): a new β₂‐adrenoceptor probe for lung imaging

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Labeling with 131I of chloroquine-analogues for the detection of ocular melanoma

Cited by 10 publications

References 17 publications

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

No-Carrier-Added Radiohalogenation Methods with Heavy Halogens

Assessing the persistence of the N–H⋯N hydrogen bonding leading to supramolecular chains in molecules related to the anti-malarial drug, chloroquine

Iodine‐125‐terbutaline (125ITB): a new β2‐adrenoceptor probe for lung imaging

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Iodine‐125‐terbutaline (¹²⁵ITB): a new β₂‐adrenoceptor probe for lung imaging